Department of Microbiology, Immunology and Transplantation, Rega Institute for Medical Research, KU Leuven, Leuven 3000, Belgium.
Hunan Provincial Key Laboratory of Clinical Epidemiology, Xiangya School of Public Health, Central South University, Changsha 410013, China.
Biochem Pharmacol. 2023 Nov;217:115862. doi: 10.1016/j.bcp.2023.115862. Epub 2023 Oct 17.
Bictegravir (BIC), a second-generation integrase strand-transfer inhibitor (INSTI) with high resilience to INSTI-resistance mutations, is integrated as a key component of Biktarvy® - a fixed-dose once-daily triple-drug regimen of bictegravir (BIC), emtricitabine (FTC) plus tenofovir alafenamide (TAF). Based on the accumulated evidence from HIV clinical trials and real-world studies, the clinical effectiveness of BIC + FTC + TAF has been proven non-inferior to other fixed-dose once-daily combinations such as dolutegravir + FTC + TAF and dolutegravir + abacavir + lamivudine. Biktarvy also shows limited drug-drug interactions and a high barrier to drug resistance. According to recent HIV guidelines, BIC + FTC + TAF is recommended as initial and long-term therapy for the treatment of HIV infection. For the pre-exposure prophylaxis, tenofovir disoproxil fumarate (TDF) or tenofovir alafenamide (TAF) remains advisable, but BIC may be possibly added to TDF or TAF. In the development of a long-acting once-monthly regimen, the novel nano-formulation of BIC + FTC + TAF could be possibly developed in the future.
比克替拉韦（BIC）是第二代整合酶链转移抑制剂（INSTI），对整合酶耐药突变具有高度抗性，是比克替拉韦片（Biktarvy®）的关键组成部分之一，这是一种每日一次的三联固定剂量药物，包含比克替拉韦（BIC）、恩曲他滨（FTC）和丙酚替诺福韦（TAF）。基于 HIV 临床试验和真实世界研究的累积证据，BIC+FTC+TAF 的临床疗效已被证明不劣于其他每日一次的固定剂量联合疗法，如多替拉韦+FTC+TAF 和多替拉韦+阿巴卡韦+拉米夫定。Biktarvy 还显示出有限的药物相互作用和较高的耐药屏障。根据最近的 HIV 指南，BIC+FTC+TAF 被推荐作为 HIV 感染的初始和长期治疗。对于暴露前预防，富马酸替诺福韦二吡呋酯（TDF）或丙酚替诺福韦（TAF）仍然是明智的选择，但 BIC 可能会添加到 TDF 或 TAF 中。在长效每月一次的方案开发中，BIC+FTC+TAF 的新型纳米制剂可能在未来得到开发。
